Гафлокс

General characteristics. Structure:

Active ingredient: 200 or 400 mg of a gatifloksatsin.

Excipients: starch corn, cellulose microcrystallic, silicon dioxide colloid, sodium carboxymethylcellulose, povidone (PVPK-30), magnesium stearate, talc, sodium krakhmalglikolit, a gipromelloza, titanium dioxide, a macrogoal (REG-6000).

Antimicrobic means of group of ftorkhinolon, effective concerning microorganisms, resistant to penicillin, cephalosporins, aminoglycosides, macroleads and tetracyclines.

Pharmacological properties:

Pharmacodynamics. Gatifloksatsin is 8-metoksiftorkhinolon, active rather wide range of gram-negative and gram-positive microorganisms.

Are sensitive to effect of drug:

Gram-positive microorganisms: Staphylococcus aureus,  Streptococcus pneumoniae, Streptococcus pyogenes.

Gram-negative microorganisms: Haemophillus influenzae, Haemophillus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Escherichia coli,  Enterobacter cloacae,  Neisseria gonorrhoeae.

Atypical activators: C. pneumoniae,  C. trachomatis,  M. pneumoniae,  L. pneumophilia, Ureaplasma.

Are moderately sensitive:

Gram-positive microorganisms:  Streptococcus milieri, Streptococcus mitior, Streptococcus agalactiae, Streptococcus dysgalactiae, Staphylococcus cohnii, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus simulans, Corynebacterium diphtheriae.

Gram-negative microorganisms: Bordetella pertussis, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter intermedius, Enterobacter sakazaki, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgerri, Providencia stuartii;

Anaerobe bacterias: Bacteroides distasonis, Bacteroides eggerthii, Bacteroides fragilis, Bacteroidesovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Fusobacterium spp., Porphyromonas spp., Porphyromonas anaerobius, Porphyromonas asaccharolyticus, Porphyromonas magnus, Prevotella spp., Propionibacterium spp., Clostridium perfringens, Clostridium ramosum.

Atypical activators: Legionella pneumophila, Caxiella burnettii.

To a gatifloksatsin such activators sensitive also, as mycobacteria of tuberculosis, H. pylori.

It inhibits enzyme a DNA gynase and ІV topoisomerase which are responsible for process of the conclusion of chromosomal DNA in a superspiral around nuclear RNA, breaks DNA biosynthesis, growth and division of bacteria; causes the expressed morphological changes (including a cell wall and membranes) and bystry death of microorganisms.

The mechanism of action of ftorkhinolon differs from effect of penicillin, cephalosporins, aminoglycosides, macroleads and tetracyclines.

Pharmacokinetics. After oral administration гатифлоксацин it is well soaked up from digestive tract, its use does not depend on reception of food. Absolute bioavailability - about 96%. The maximum concentration is reached in 1 - 2 h after reception and at doses of 200 mg and 400 mg represents 2,0±0,4 mkg/ml and 3,8±1,0 mkg/ml, respectively. Equilibrium concentration is reached for the third day of administration of drug. Average equilibrium concentration and concentration in a blood plasma at daily reception of a dose of 400 mg disposable represents about 4,2 g/ml and 0,4 g/ml, respectively.

20% of a gatifloksatsin irrespective of concentration contact proteins of plasma.

Gatifloksatsin well gets into the majority of body tissues and is quickly distributed on biological liquids: high concentration are created in pulmonary tissue, a mucous membrane of bronchial tubes, adnexal nasal cavities, in alveolar macrophages, tissues of a middle ear, skin, fabrics and a secret of a prostate, saliva, bile, semen, a vagina, a uterus, Indo-and to a myometrium, uterine tubes, ovaries

Gatifloksatsin is brought by kidneys. The elimination half-life represents from 7 to 14 h and does not depend on a dose and a course of treatment. The renal clearance does not depend on a dose and is in limits of 124 - 161 ml/min. Gatifloksatsin is brought by glomerular filtering and canalicular secretion. More than 70% to a gatifloksatsin are removed with urine in 48 h after reception. Drug also gives in to the minimum hepatic and/or intestinal elimination as 5 its % appear in excrements in not changed look. Less than 1% are removed with urine in the form of metabolites of ethylene diamine and methylethylene diamine.

In tests for animals гатифлоксацин freely gets through a placenta and comes to breast milk.

Indications to use:

Indications to use of drug of Gafloks are: infections at patients are aged more senior than 18 years caused by activators, sensitive to a gatifloksatsin: respiratory tracts (including an acute bronchitis, abscess of lungs, persistent respiratory infections in an aggravation phase, cystous fibrosis, pneumonia); kidneys and uric ways (including the acute and chronic pyelonephritis, prostatitis, cystitis, persistent infections of urinogenital system including complicated); skin and soft tissues; bones and joints; digestive tract; postoperative, sepsis, peritonitis; at patients of an oncological profile.

Route of administration and doses:

Administration of drug does not depend on meals.

At acute and chronic bronchitis in a phase of an aggravation, pneumonia, infections of skin and a hypodermic fatty tissue, acute pyelonephritis and the complicated infections of uric ways — 400 mg of 1 times a day or on 200 mg 2 times a day within 7–10 days.

At acute sinusitis — 400 mg of 1 times a day or on 200 mg 2 times a day for 7–14 days; at uncomplicated infections of uric ways (cystitis) — in an initial dose of 400 mg, then 200 mg of 1 times a day within 3 days; at an uncomplicated gonococcal urethritis at men, a gonococcal endocervicitis and a proctitis at women — 400 mg once.

As гатифлоксацин it is allocated with kidneys, the dose of a gatifloksatsin needs to be korrigirovat for patients with clearance of creatinine <30 ml/min., including being on dialysis. The recommended dose of a gatifloksatsin for such patients — on 400 mg each 2 days, for the 3rd day — a break, since 4th day — on 400 mg each 48 h. For the patients who are on a chronic hemodialysis, the drug is administered after dialysis session.

At single use of drug need for dose adjustment does not arise.

Features of use:

Gatifloksatsin can prolong QT an electrocardiogram interval therefore it is not appointed to patients with the interval prolonged by QT, a hypopotassemia which is not adjusted, and to patients who receive antiarrhythmic means of a class ІА (quinidine, новокаинамид) or to a class ІІІ (Amiodaronum, соталол).

As well as other hinolona, гатифлоксацин with care appoint at pathology of the central nervous system in the anamnesis: at mental diseases, epilepsy, heavy atherosclerosis of vessels of a brain (risk of disturbance of blood supply, a stroke), and also at renal failures, when clearance of creatinine less than 40 ml/min. (necessary control of concentration of drug in a blood plasma).

As at use of drug disturbance of level of glucose in blood, including symptomatic hyper - and a hypoglycemia, especially at the patients sick with diabetes who receive accompanying treatment by hypoglycemic means or insulin is observed, constant control of this level in blood is surely necessary.

If heavy diarrhea develops, it is necessary to exclude pseudomembranous colitis (at which hinolona are contraindicated).

Drug can cause dizziness that should be considered to patients who work with potentially dangerous mechanisms, direct vehicles, or are connected with activity which needs vigilance and coherence of actions.

Drug is removed by kidneys therefore the risk of toxic reactions is increased at patients with a renal failure. As people of advanced years (65 years are more senior) are more inclined to such reactions, it is necessary to select doses with care, and also it is necessary to control functions of kidneys.

Do not use this drug during pregnancy and feeding by a breast.

Side effects:

Most often from side effects from drug of Gafloks there are vomiting, diarrhea, a vaginitis, an abdominal pain, a headache, dizziness; more rare — taste disturbance, allergic reactions, a fever, fever, a dorsodynia, a stethalgia, tachycardia, a lock, dyspepsia, a glossitis, candidiasis of an oral cavity, stomatitis, ulcers of a mucous membrane of an oral cavity, peripheral hypostases, sleeplessness, paresthesia, a tremor, vasodilatation, dizziness, диспноэ, pharyngitis, perspiration, a vision disorder, a sonitus, a dysuria and a hamaturia. The photosensitization was noted with the same frequency, as when using placebo. Hinolona can cause disturbances from TsNS, including a hyperexcitability, concern, sleeplessness, hallucinations, etc.

Interaction with other medicines:

At introduction with drug of Gafloks through one catheter consistently of other drugs it needs to be washed out before introduction of a gatifloksatsin by means of solution which is compatible with gatifloksatsiny and the used drugs.

As well as at purpose of other hinolon, at patients with a diabetes mellitus it can be noted symptomatic hyper - or a hypoglycemia (is more often at simultaneous treatment by peroral gipoglikemiziruyushchy drugs, for example Glyburidum, or insulins therapy. At these patients it is recommended to a thicket to control glucose level in a blood plasma.

Gatifloksatsin can cause lengthening of an interval of Q-T on an ECG in some patients. In view of insufficient clinical experience гатифлоксацин it is not necessary to apply when lengthening an interval of Q-T, at patients with a hypercalcemia and at those who receive antiarrhytmic means of the class IA (quinidine, procaineamide) or the III class (Amiodaronum, соталол). Pharmacokinetic researches for the gatifloksatsin and drugs capable to extend Q–T interval (such as цизаприд, erythromycin), antipsychotic means and tricyclic antidepressants therefore гатифлоксацин it is necessary to take with caution at simultaneous use with these drugs are not conducted.

Reception of a gatifloksatsin in 1 h after Cimetidinum H2 receptors blocker (in 1 times a day in a dose of 200 mg) did not exert impact on pharmacokinetics of a gatifloksatsin.

Gatifloksatsin does not influence system clearance of midazolam at in introduction. Midazolam in a daily dose of 0,0145 mg/kg did not influence pharmacokinetics of a gatifloksatsin.

Simultaneous use of a gatifloksatsin and warfarin did not influence pharmacokinetics of any of drugs, the prothrombin time did not change.

At simultaneous use of a gatifloksatsin and Glyburidum for patients with a diabetes mellitus considerable changes of pharmacokinetics of drugs are noted, glucose level in blood on an empty stomach did not change.

At simultaneous use of a gatifloksatsin and digoxin considerable changes of pharmacokinetics of a gatifloksatsin are not revealed, however at some patients concentration of digoxin in blood increased. Control of concentration of digoxin in a blood plasma and if necessary — digoxin dose adjustment is required.

The system clearance of a gatifloksatsin considerably increases at simultaneous use of a gatifloksatsin and probenetsid.

At patients who received warfarin considerable changes of a blood clotting time at simultaneous use of a gatifloksatsin are not revealed. However because some hinolona strengthen effect of warfarin and similar means, at purpose of a similar combination control of a prothrombin time is required.

At simultaneous use with NPVP hinolona can increase risk of development of side effects from TsNS, including spasms.

Contraindications:

Contraindications to use of drug of Gafloks are: hypersensitivity to a gatifloksatsin and other components of drug, other hinolona; period of pregnancy and feeding by a breast, and also pediatric practice.

Overdose:

In case of overdose of drug of Gafloks the patient has to is under medical control with tracking of all vital functions, including the cardiogram. Carry out the supporting and symptomatic treatment - washing a deludka, use of vomitives, introduction of a large amount of liquid. The hemodialysis and peritoneal dialysis are inefficient.

Storage conditions:

To store in unavailable to children, the dry place at a temperature below 30 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in one blister strip packaging in a cardboard pack. On 10 blister strip packagings in a cardboard pack.